| Modulation of NSAID-induced antinociceptive and anti-inflammatory effects by alpha2-adrenoceptor agonists with gastroprotective effects. | |
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MedLine Citation:
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PMID: 12269398 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Tizanidine, an alpha2-adrenergic receptor agonist with myospasmolytic action, is indicated for the treatment of back pain either as monotherapy or in combination with nonsteridal anti-inflammatory drugs (NSAIDs). Tizanidine (0.25-1.0 mg/kg) significantly produced analgesic and anti-inflammatory effect in acetic acid induced writhing in mice and carrageenan-induced paw edema in rats, respectively. The effects were comparable with clonidine (0.25 and 0.50 mg/kg), another alpha2-agonist. Yohimbine (1 mg/kg), alpha2-adrenergic antagonist reversed the effect of tizanidine. Tizanidine (0.25 mg/kg) and clonidine (0.25 mg/kg) significantly potentiated the antinociceptive and anti-inflammatory effect of NSAIDs (nimesulide, meloxicam and naproxen). Tizanidine (1 mg/kg) did not alter basal pH, acidity (free and total) of gastric content and did not produce any mucosal injury in fasted rats. Tizanidine (1 mg/kg) significantly reduced meloxicam (UD50 3.21 mg/kg), nimesulide (UD50 24.52 mg/kg) and naproxen (UD50 14.10 mg/kg)-induced ulcerogenic effect (ulcer index, pH and free/total acidity). It is expected that tizanidine exerted gastrotprotection through stimulation of gastric and central alpha2-adrenergic receptors. Present investigation suggested that tizanidine not only enhance the analgesic and anti-inflammatory effect of NSAIDs but also improved gatstrointestinal tolerability of NSAIDs through modulation of central alpha-2-receptors. From this study, it can be speculated that tizanidine and NSAID combination therapy would prove to be a novel approach to treat nociceptive/inflammatory conditions with improved gastric tolerability of NSAIDs. |
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Authors:
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Naveen K Jain; Shrinivas K Kulkarni; Amarjit Singh |
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Publication Detail:
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Type: Comparative Study; Journal Article |
Journal Detail:
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Title: Life sciences Volume: 70 ISSN: 0024-3205 ISO Abbreviation: Life Sci. Publication Date: 2002 May |
Date Detail:
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Created Date: 2002-09-24 Completed Date: 2002-10-04 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0375521 Medline TA: Life Sci Country: England |
Other Details:
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Languages: eng Pagination: 2857-69 Citation Subset: IM |
Affiliation:
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Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic alpha-Agonists
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therapeutic use* Animals Anti-Inflammatory Agents, Non-Steroidal / therapeutic use* Clonidine / analogs & derivatives*, therapeutic use Drug Synergism Drug Therapy, Combination Mice Naproxen / therapeutic use Pain / drug therapy* Rats Rats, Wistar Receptors, Adrenergic, alpha-2 / metabolism* Stomach Ulcer / prevention & control* Sulfonamides / therapeutic use Thiazines / therapeutic use Thiazoles / therapeutic use Yohimbine / therapeutic use |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic alpha-Agonists; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Receptors, Adrenergic, alpha-2; 0/Sulfonamides; 0/Thiazines; 0/Thiazoles; 146-48-5/Yohimbine; 22204-53-1/Naproxen; 4205-90-7/Clonidine; 51322-75-9/tizanidine; 51803-78-2/nimesulide; 71125-38-7/meloxicam |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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